Deoxypodophyllotoxin (DPT) is a kind of lignan compound isolated from nature as like podophyllotoxin. It has been reported that podophyllotoxin shows a cytotoxicity to some kinds of cancer cells. Etoposide, a derivative of podophyllotoxin, is now widely used for clinical purposes [see, I. Jardine; In Anticancer Agents based on Natural Product Models; J. M. Cassidy et al.; Eds.; Academic Press: New York, 319-351, 1980], and is known to show a special effect against SCLC (Small Cell Lung Cancer), malignant lymphoma, etc. [see, T. Utsugi et al.; cancer research, 56, 2809, 1996].
However, differently from podophyllotoxin, researches for deoxypodophyllotoxin (DPT) and derivatives thereof as an anticancer agent have not been carried out yet. Anticancer researches for this compound still remain at the step of cytotoxicity. San Feliciano et al., Planta Medica 59, 247, 1993; Arch. Pharm. 327, 175, 1994; D. B. M. Wickramaratne et al., Planta Medica, 61, 80, 1995; J. J. Chen et al., Planta Medica 62, 528, 1996; and M. Novelo et al., J. Nat. Pro. 56(10), 1728, 1993 reported that this compound shows a potent cytotoxicity against tumor cells, and R. S. Gupta et al., Cancer Research 43, 505-512, 1983; and J. D. Loike et al., Cancer Research 38, 2688-2693, 1978 reported that the cytotoxicity causes an inhibition of cell division through an inhibition of microtubule assembly (IC50; 0.6 mM). Further, T. Terada et al., Chem. Pharm. Bull., 40, 2720-2727, 1992 reported that mouse leukemia cell line L1210 was transplanted into CDF1 mouse, and in that case deoxypodophyllotoxin exhibited an extension effect of life span in about 12% compared with the negative control.
After the above reports, no more researches for the anticancer activity of deoxypodophyllotoxin derivatives have been carried out. This seems to be because deoxypodophyllotoxin does not show any anticancer activity in animal models due to its low bioavailability.